Imvelaphi

I-Atorvastatin Calcium yi-inhibitor enamandla ye-HMG-CoA reductase enexabiso le-IC50 le-150 nM[1].
I-HMG-CoA reductase yi-enzyme ephambili yemevalonate indlela evelisa i-cholesterol.I-HMG-CoA yi-enzyme yokunciphisa izinga kwaye ibalulekile ekunciphiseni amanqanaba e-cholesterol yegazi.I-HMG-CoA reductase ifumaneka kwi-endoplasmic reticulum kwaye iqulethe iindawo ezisibhozo ze-transmembrane.I-inhibitors ye-HMG-CoA reductase inokubangela ukuba i-LDL (i-low density lipoprotein) ibonakaliswe kwisibindi.Ikhokelela ekunyuseni amanqanaba e-catabolism ye-plasma ye-LDL kunye nokunciphisa ukuxinwa kwe-cholesterol ye-plasma eyona nto ibalulekileyo kwi-atherosclerosis.I-HMG-CoA reductase idlala indima ebalulekileyo kwi-cholesterol synthesis.I-HMG-CoA yiyona nto ekujoliswe kuyo kwiziyobisi zokunciphisa i-cholesterol.I-HMG-CoA reductase ikwayi-enzyme ebalulekileyo yophuhliso.Umsebenzi we-HMG-CoA reductase unxulumene neziphene zokufuduka kweeseli zentsholongwane.Ukuthintelwa komsebenzi wayo kunokukhokelela kukopha kwi-intracerebral [1].
I-Atorvastatin yi-HMG-CoA reductase inhibitor enexabiso le-IC50 le-154 nM.Iyasebenza ekunyangeni i-dyslipidemias kunye ne-hypercholesterolemia [1].Unyango lwe-Atorvastatin kwi-40 mg yehlisa i-cholesterol epheleleyo ye-40% emva kweentsuku ze-40.[1]Ikwasetyenziselwa ukunyanga izigulane ze-coronary okanye i-stroke ezinamaqondo aqhelekileyo e-cholesterol.[2]I-Atorvastatin iphinda yehlise i-low density lipoprotein apheresis kwizigulana ngokubangela i-LDL-receptors expression.
I-metabolized kwi-metabolites ezininzi ezibalulekileyo kwimpembelelo yezenzo zonyango nge-CYP3A4 (cytochrome P450 3A4).[3]
IiReferensi:
[1].van Dam M, Zwart M, de Beer F, Smelt AH, Prins MH, Trip MD, Havekes LM, Lansberg PJ, Kastelein JJ: Ukusebenza kwexesha elide kunye nokhuseleko lwe-atorvastatin kunyango olunzima lwe-III kunye ne-dyslipidaemia edibeneyo.Intliziyo 2002, 88 (3): 234-238.
[2].I-Sever PS, i-Dahlof B, i-Poulter NR, i-Wedel H, i-Beevers G, i-Caulfield M, i-Collins R, i-Kjeldsen SE, i-Kristinsson A, i-McInnes GT et al: Uthintelo lweziganeko ze-coronary kunye ne-stroke kunye ne-atorvastatin kwizigulane ezine-hypertension ezinomndilili okanye ophantsi-kunokuba -i-avareji ye-cholesterol concentrations, kwi-Anglo-Scandinavian Cardiac Outcomes Trial--Lipid Lowering Arm (ASCOT-LLA): uvavanyo olulawulwa ngamathuba amaninzi.Lancet 2003, 361(9364): 1149-1158.
[3].Lennernas H: I-pharmacokinetics yeklinikhi ye-atorvastatin.I-Clin Pharmacokinet 2003, 42 (13): 1141-1160.

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